EP1577308A2 - Nicht-steroidale polyzyklische Sulfamat-Derivate, deren Herstellung und deren Verwendung als Östron Sulfatase Inhibitoren - Google Patents

Nicht-steroidale polyzyklische Sulfamat-Derivate, deren Herstellung und deren Verwendung als Östron Sulfatase Inhibitoren Download PDF

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Publication number
EP1577308A2
EP1577308A2 EP05000983A EP05000983A EP1577308A2 EP 1577308 A2 EP1577308 A2 EP 1577308A2 EP 05000983 A EP05000983 A EP 05000983A EP 05000983 A EP05000983 A EP 05000983A EP 1577308 A2 EP1577308 A2 EP 1577308A2
Authority
EP
European Patent Office
Prior art keywords
compound
sulphamate
steroidal
independently selected
ring
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP05000983A
Other languages
English (en)
French (fr)
Other versions
EP1577308A3 (de
Inventor
Michael John Reed
Barry Victor Lloyd Potter
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sterix Ltd
Original Assignee
Sterix Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sterix Ltd filed Critical Sterix Ltd
Publication of EP1577308A2 publication Critical patent/EP1577308A2/de
Publication of EP1577308A3 publication Critical patent/EP1577308A3/de
Withdrawn legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/06—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2
    • C07D311/08—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring
    • C07D311/16—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring substituted in position 7
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
    • A61K31/37—Coumarins, e.g. psoralen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens

Definitions

  • sulphamate group of the compound were to be replaced with a sulphate group to form a sulphate compound then that sulphate compound would be hydrolysable by an enzyme having steroid sulphatase (E.C. 3.1.6.2) activity.
  • a non-steroidal compound according to the present invention in the manufacture of a pharmaceutical for inhibiting oestrone sulphatase.
  • the alkyl group(s) in Formula (A) or Formula (B) can be any suitable linear or branched alkyl group which may be saturated or unsaturated and/or substituted or non-substituted.
  • the alkyl group may even be a cyclic alkyl group.
  • at least two of R 1-6 are linked to form a further cyclic component.
  • the compounds of the present invention have reduced, or even minimal or no, oestrogenic activity.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrane Compounds (AREA)
EP05000983A 1996-02-16 1997-02-17 Nicht-steroidale polyzyklische Sulfamat-Derivate, deren Herstellung und deren Verwendung als Östron Sulfatase Inhibitoren Withdrawn EP1577308A3 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB9603325 1996-02-16
GBGB9603325.3A GB9603325D0 (en) 1996-02-16 1996-02-16 A compound
EP97903494A EP0880514B1 (de) 1996-02-16 1997-02-17 Nicht-steroidale polyzyklische sulfamat-derivate, deren herstellung und deren verwendung als östron sulfatase inhibitoren

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
EP97903494A Division EP0880514B1 (de) 1996-02-16 1997-02-17 Nicht-steroidale polyzyklische sulfamat-derivate, deren herstellung und deren verwendung als östron sulfatase inhibitoren

Publications (2)

Publication Number Publication Date
EP1577308A2 true EP1577308A2 (de) 2005-09-21
EP1577308A3 EP1577308A3 (de) 2007-08-29

Family

ID=10788910

Family Applications (2)

Application Number Title Priority Date Filing Date
EP97903494A Expired - Lifetime EP0880514B1 (de) 1996-02-16 1997-02-17 Nicht-steroidale polyzyklische sulfamat-derivate, deren herstellung und deren verwendung als östron sulfatase inhibitoren
EP05000983A Withdrawn EP1577308A3 (de) 1996-02-16 1997-02-17 Nicht-steroidale polyzyklische Sulfamat-Derivate, deren Herstellung und deren Verwendung als Östron Sulfatase Inhibitoren

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EP97903494A Expired - Lifetime EP0880514B1 (de) 1996-02-16 1997-02-17 Nicht-steroidale polyzyklische sulfamat-derivate, deren herstellung und deren verwendung als östron sulfatase inhibitoren

Country Status (14)

Country Link
US (1) US6239169B1 (de)
EP (2) EP0880514B1 (de)
JP (2) JP4047927B2 (de)
CN (3) CN100376244C (de)
AT (1) ATE293614T1 (de)
AU (1) AU1804197A (de)
CY (1) CY2559B1 (de)
DE (1) DE69733061T2 (de)
ES (1) ES2238078T3 (de)
GB (1) GB9603325D0 (de)
IL (1) IL125752A (de)
NZ (1) NZ331326A (de)
PT (1) PT880514E (de)
WO (1) WO1997030041A1 (de)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9604709D0 (en) * 1996-03-05 1996-05-01 Imperial College A compound
US6083978A (en) * 1996-03-05 2000-07-04 Sterix Limited Compounds with a sulfamate group
US6011024A (en) 1991-08-28 2000-01-04 Imperial College Of Science Technology & Medicine Steroid sulphatase inhibitors
US6903084B2 (en) 1991-08-28 2005-06-07 Sterix Limited Steroid sulphatase inhibitors
GB9118478D0 (en) * 1991-08-29 1991-10-16 Imperial College Steroid sulphatase inhibitors
US6476011B1 (en) 1991-08-28 2002-11-05 Sterix Limited Methods for introducing an estrogenic compound
US6506792B1 (en) 1997-03-04 2003-01-14 Sterix Limited Compounds that inhibit oestrone sulphatase and/or aromatase and methods for making and using
US6921776B1 (en) * 1996-02-16 2005-07-26 Sterix Limited Compound
US20040127473A1 (en) * 1996-12-05 2004-07-01 Reed Michael John Compound
GB2331988B (en) 1997-12-04 2003-04-16 Imperial College Polycyclic sulphamate inhibitors or oestrone sulphatase
GB9807779D0 (en) 1998-04-09 1998-06-10 Ciba Geigy Ag Organic compounds
JP2000309599A (ja) 1999-04-13 2000-11-07 Kyowa Hakko Kogyo Co Ltd エストラ−１，３，５（１０），１６−テトラエン誘導体
US7078395B1 (en) 1999-06-16 2006-07-18 Sterix Limited Methods for treating or preventing cancer by preventing, inhibiting or arresting cell cycling
IL145995A0 (en) 1999-04-30 2002-07-25 Sterix Ltd Use
US7335650B2 (en) 2000-01-14 2008-02-26 Sterix Limited Composition
WO2002015910A1 (en) * 2000-08-18 2002-02-28 Sterix Limited 2-substituted estradiol derivative for inhibiting superoxid dismutase
US6632835B2 (en) * 2001-02-22 2003-10-14 Nanodesign Inc. Dibenzo[c]chromen-6-one derivatives as anti-cancer agents
GB0511190D0 (en) * 2005-06-01 2005-07-06 Sterix Ltd Use
GB0624105D0 (en) * 2006-12-01 2007-01-10 Sterix Ltd Use
BRPI0817045A2 (pt) 2007-09-17 2015-03-24 Preglem Sa Tratamento de condições estrogênio-dependentes em mulheres pré-menopáusicas
FR2942226B1 (fr) * 2009-02-13 2011-02-25 Ipsen Pharma Sas Nouveau polymorphe cristallin du 6-oxo+6,7,8,9,10,11-hexahydrocyclohepta°c!chromen-3-yl sulfamate
FR2942225B1 (fr) * 2009-02-13 2013-03-01 Ipsen Pharma Sas Variete i du 6-oxo-6,7,8,9,10,11-hexahydroclyclohepta5°c!chromen-3 yl sulfamate de granulometrie reduite
US8691281B2 (en) 2009-02-13 2014-04-08 Ipsen Pharma S.A.S. Solid pharmaceutical composition containing 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta (C)chromen-3-yl sulfamate and polymorphs thereof
RU2011137516A (ru) * 2009-02-13 2013-03-20 Ипсен Фарма С.А.С. ТВЕРДАЯ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ 6-ОКСО-6,7,8,9,10,11-ГЕКСАГИДРОЦИКЛОГЕПТА[c]ХРОМЕН-3-ИЛСУЛЬФАМАТ И ЕГО ПОЛИФОРМЫ
WO2011151061A1 (en) 2010-06-03 2011-12-08 Ipsen Pharma S.A.S. Al035301, a biomarker for breast cancer
CN104606186B (zh) * 2014-11-19 2017-09-12 北京工业大学 氟代7‑羟基香豆素化合物在蛋白激酶抑制剂或/和抗肿瘤药物中的应用
EP3810128B1 (de) 2018-06-19 2022-08-03 Universidad Pablo de Olavide Zusammensetzungen zur behandlung und/oder prävention von proteinaggregationserkrankungen
RU2752086C1 (ru) * 2020-04-27 2021-07-22 Общество С Ограниченной Ответственностью "Валента-Интеллект" Новое соединение [2-(диметиламино)-2-фенилбутил]-3,4,5-триметоксибензоата 4-метил-2н-хромен-2-он-7-илсульфат и его применение
CN112480055B (zh) * 2020-12-11 2022-10-21 肇庆学院 一种橙皮素衍生物及其合成方法与用途

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3243158A1 (de) 1982-11-23 1984-05-24 Basf Ag, 6700 Ludwigshafen Neue sulfonsaeureester von hydroxycumarinen, ihre herstellung und sie enthaltende arzneimittel
FR2543140B1 (fr) 1983-03-24 1985-06-21 Cortial Nouveaux acides flavone-carboxyliques-4', leur methode de preparation et leur application en therapeutique
PT94305B (pt) * 1989-06-12 1997-02-28 Robins Co Inc A H Processo para a preparacao de compostos tendo um ou mais radicais aminossulfoniloxi uteis como produtos farmaceuticos
US5192785A (en) * 1989-09-03 1993-03-09 A. H. Robins Company, Incorporated Sulfamates as antiglaucoma agents
US5025031A (en) * 1989-11-30 1991-06-18 A. H. Robins Co., Inc. Aryl and aryloxyalkyl sulfamate esters useful as anticonvulsants
US6011024A (en) 1991-08-28 2000-01-04 Imperial College Of Science Technology & Medicine Steroid sulphatase inhibitors
GB9118478D0 (en) 1991-08-29 1991-10-16 Imperial College Steroid sulphatase inhibitors
US6083978A (en) 1996-03-05 2000-07-04 Sterix Limited Compounds with a sulfamate group

Also Published As

Publication number Publication date
CN100376244C (zh) 2008-03-26
JP4047927B2 (ja) 2008-02-13
CN1216044A (zh) 1999-05-05
AU1804197A (en) 1997-09-02
JP2008001723A (ja) 2008-01-10
PT880514E (pt) 2005-08-31
IL125752A (en) 2007-07-04
CN1701790A (zh) 2005-11-30
US6239169B1 (en) 2001-05-29
EP0880514A1 (de) 1998-12-02
ES2238078T3 (es) 2005-08-16
JP4949982B2 (ja) 2012-06-13
CY2559B1 (en) 2008-07-02
EP1577308A3 (de) 2007-08-29
DE69733061T2 (de) 2005-08-18
CN1210272C (zh) 2005-07-13
DE69733061D1 (de) 2005-05-25
WO1997030041A1 (en) 1997-08-21
EP0880514B1 (de) 2005-04-20
ATE293614T1 (de) 2005-05-15
CN1989961A (zh) 2007-07-04
JP2000504717A (ja) 2000-04-18
IL125752A0 (en) 1999-04-11
GB9603325D0 (en) 1996-04-17
NZ331326A (en) 2000-03-27

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